CGRPR/CRE Luciferase Reporter HEK293 Cell Line

Catalog #

78325

$10,340 *

Size: 2 vials

Qty

Bulk/Custom

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*US Pricing only. For international pricing, please contact your local distributor.

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Description

Recombinant HEK293 cell line stably expressing full-length human calcitonin receptor-like receptor (CALCRL/CRLR/CLR; accession number: NM_005795) and firefly luciferase under the control of a multimerized cAMP response element (CRE). This cell line can be used to measure the EC₅₀ and IC₅₀ of CGRP receptor agonists and antagonists using luciferase reporter activity as read-out.

Interested in screening and profiling inhibitors, blocking antibodies, or activators of CGRPR without the need to purchase and license the cell line? Check out our Cell Signaling Pathway Screening.

Purchase of this cell line is for research purposes only; commercial use requires a separate license. View the full terms and conditions.

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Synonyms

Calcitonin gene-related peptide type 1 receptor, CGRP type 1 receptor, Calcitonin receptor-like receptor, CRLR, CGRPR, LMPHM8, CALCRL, CLR

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Product Data Gallery

Cell surface expression of human CALCRL in CGRPR/CRE Luciferase Reporter HEK293 Cell Line.

Dose response of CGRPR/CRE Luciferase Reporter HEK293 Cell Line to the agonists α-CGRP and β-CGRP.

Dose response of CGRPR/CRE Luciferase Reporter HEK293 Cell Line to the small molecule antagonist Rimegepant.

Dose response of CGRPR/CRE Luciferase Reporter HEK293 Cell Line to the anti-CGRP Eptinezumab.

Dose response of CGRPR/CRE Luciferase Reporter HEK293 Cell Line to the anti-CGRP antibody Galcanezumab.

Product Info

Storage and Usage

Citations

Host Cell Line

HEK293, Human Embryonic Kidney, epithelial-like cells, adherent

Species

Human

Supplied As

Each vial contains >1 x 10⁶ cells in 1 ml of Cell Freezing Medium (BPS Bioscience #79796)

Materials Required But Not Supplied

Materials Required for Cell Culture

Name	Ordering Information
Thaw Medium 1	BPS Bioscience #60187
Growth Medium 1G	BPS Bioscience #79544

Materials Required for Cellular Assay

Name	Ordering Information
Thaw Medium 1	BPS Bioscience #60187
Growth Medium 1G	BPS Bioscience #79544
MEM medium for preparing assay medium	Hyclone #SH30024.01
Bovine Serum Albumin (BSA, protease free)	Sigma #A4919
Human α-CGRP	Sigma #C0167
Human β- CGRP	Cayman Chemical #24725
Rimegepant	Cayman Chemical #26338
Zavegepant (Vazegepant) Hydrochloride
Eptinezumab	Invitrogen #MA5-42119
Galcanezumab	Invitrogen #MA5-42106
Anti-CALCRL antibody	Aviva #APR42260
PE Donkey Anti-Rabbit Antibody	Biolegend #406421
ONE-Step™ Luciferase Assay System	BPS Bioscience #60690
Luminometer

Genbank #

NM_005795

UniProt #

Q16602

Mycoplasma Testing

The cell line has been screened to confirm the absence of Mycoplasma species.

Background

Calcitonin gene-related peptide (CGRP) receptor is a G-protein coupled receptor with three components: calcitonin receptor-like receptor (CALCRL), receptor activity-modifying protein (RAMP1) and CGRP-receptor component protein (CRCP). RAMP1 is required for both the trafficking of the calcitonin-like receptor to the plasma membrane and the coupling of the receptor with CGRP agonist. CRCP is involved in the association between the CGRP receptor and the G protein. Upon ligand binding, the complex interacts with the G protein, the Gαs subunit dissociates from the complex and activates adenylyl cyclase, which produces cAMP. Elevation of the intracellular concentration of cAMP stimulates cAMP-dependent signaling pathways, ultimately resulting in transcription factor cAMP response element binding protein (CREB) to bind to the CRE promoter and induce gene expression.

Figure 1: Mechanism of action of CGRP.

Preclinical evidence suggests that during a migraine, activated sensory neurons in the trigeminal ganglion release CGRP from their projecting nerve endings located within the meninges. The released CGRP then binds and activates CGRP receptors causing vasodilation and plasma extravasation. Further evidence comes from the observation that intravenous administration of α-CGRP induces a headache in susceptible individuals. Recent breakthroughs in understanding the role of CGRP in migraine has led to the development of a novel class of CGRP antagonist biologics that promise significant improvement over conventional pharmacotherapy

Storage/Stability

Cells are shipped in dry ice and should immediately be thawed or stored in liquid nitrogen upon receipt. Do not use a -80°C freezer for long term storage.

Growth Media

For best results, it is highly recommended to use these validated and optimized media from BPS Bioscience. Other preparations or formulations of media may result in suboptimal performance.

Media Required for Cell Culture

Thaw Medium 1 (BPS Bioscience #60187): MEM medium supplemented with 10% FBS, 1% non-essential amino acids, 1 mM Na pyruvate, 1% Penicillin/Streptomycin.

Growth Medium 1G (BPS Bioscience #79544): MEM medium supplemented with 10% FBS, 1% non-essential amino acids, 1 mM Na pyruvate, 1% Penicillin/Streptomycin plus 400 µg/ml of Geneticin and 50 µg/ml of Hygromycin B.

Media Required for Functional Cellular Assay

Thaw Medium 1 (BPS Bioscience #60187): MEM medium supplemented with 10% FBS, 1% non-essential amino acids, 1 mM Na pyruvate, 1% Penicillin/Streptomycin.

Assay Medium: MEM + 1% BSA (protease free).

Applications

Screen for activators or inhibitors of CGRP receptor for immunotherapy research and drug discovery.
Screen for anti-CGRP antibodies.

Shipping Temperature

-80°C

Notes

License Disclosure
Visit bpsbioscience.com/license for the label license and other key information about this product.

Troubleshooting Guide
Visit bpsbioscience.com/cell-line-faq for detailed troubleshooting instructions. For all further questions, please email [email protected].

Warnings

Avoid freeze/thaw cycles

Scientific Category

Neuroscience

Regulatory Status

Research Use Only